A Series of 2,4(1H,3H)-Quinazolinedione Derivatives: Synthesis and Biological Evaluation as Potential Anticancer Agents

Title:A Series of 2,4(1H,3H)-Quinazolinedione Derivatives: Synthesis and Biological Evaluation as Potential Anticancer Agents

Volume: 13 Issue: 1

Author(s): Hulya Akgun, Demet Us Yilmaz, Rengul Cetin Atalay and Damla Gozen

Affiliation:

Keywords: Quinazoline, quinazoline-2, 4(1H, 3H)-dione, piperazine, cytotoxicity, anticancer, sulforhodamine B method.

Abstract: A series of 6,7-disubstituted-3-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}quinazoline- 2,4(1H,3H)-dione derivatives (7-34) were synthesized and their structures were elucidated on the basis of analytical and spectral (UV, IR, ¹H-NMR, ¹³C-NMR and MS) data. These synthesized compounds were evaluated for their in vitro cytotoxicities against a panel of three human cancer cell lines. According to the cytotoxicity screening results, 3-{2-[4-(4-chlorobenzyl)piperazin-1-yl]-2-oxoethyl} quinazoline-2,4(1H,3H)-dione (7) presented the highest activity against HUH-7, MCF-7 and HCT-116 cell line with the IC₅₀ values of 2.5, 6.8 and 4.9 µM, respectively.

Cite this article as:

Akgun Hulya, Us Yilmaz Demet, Cetin Atalay Rengul and Gozen Damla, A Series of 2,4(1H,3H)-Quinazolinedione Derivatives: Synthesis and Biological Evaluation as Potential Anticancer Agents, Letters in Drug Design & Discovery 2016; 13 (1) . https://dx.doi.org/10.2174/1570180812666150529204909